849335-54-2Relevant academic research and scientific papers
Design, synthesis, and SAR study of novel 4,5-dihydropyrazole-Thiazole derivatives with anti-inflammatory activities for the treatment of sepsis
Cao, Peichang,Duan, Yajun,Fang, Mengyuan,Han, Jihong,Li, Qing-Shan,Xu, Huajian,Yang, Xiaoxiao,Zhang, Zhen,Zou, Tingfeng
, (2021/08/17)
Systemic inflammatory response syndrome is a major feature of sepsis which is one of the major causes of death worldwide. It has been reported that 3,5-diaryl-4,5-dihydropyrazole and thiazole derivatives have many biological functions, especially in the aspect of anti-inflammation. According to the strategy of pharmacophore combination, we introduced thiazole moiety into dihydropyrazole skeleton to design and synthesize a novel series of 2-(3,5-diphenyl-4,5-dihydro-1H-pyrazol-1-yl)-4-methylthiazole derivatives, and evaluated their anti-inflammatory activities for sepsis treatment. Preliminary structure?activity relationship (SAR) analysis was conducted by their inhibitory activities against nitric oxide (NO) release in LPS-induced RAW264.7 cells, and the optimal compound E26 exhibited more potent anti-inflammatory activity than the positive control treatment indomethacin and dexamethasone. In further mechanism study, our results showed that compound E26 significantly suppressed the production of interleukin-1β (IL-1β), tumor necrosis factor-α (TNF-α), NO and inhibited the expressions of inducible nitric oxide synthase (iNOS), cyclooxygenase-2 (COX-2) through blocking MAPKs signaling pathway. In addition, in vivo administration of compound E26 resulted in a significant improvement of LPS-induced sepsis in C57BL/6J mice, with reducing toxicity in multiple organs. Taken together, this study demonstrated the compound E26 could be a promising agent for the treatment of sepsis.
Palladium Nanoparticles-Catalyzed Synthesis of Indanone Derivatives via Intramolecular Reductive Heck Reaction
Parveen, Naziya,Sekar, Govindasamy
, p. 4581 - 4595 (2019/09/03)
An efficient protocol for the straightforward, single-step synthesis of 3-aryl-1-indanones from 2′-iodochalcone via reductive Heck reaction using phosphine free, stable and reusable binaphthyl stabilized palladium nanoparticle (Pd-BNP) as a catalyst has been described. An immense array of substrate scope with electron-rich and deficient 2′-iodochalcones have been synthesized. Further derivatization of product indanones have been achieved successfully. The heterogeneous nature of the Pd-BNP has been validated by centrifugation test and mercury poisoning experiment. Pd-BNP has been successfully recycled up to 5 cycles without any significant loss in reaction yield and particle size of nanoparticles, confirmed by TEM analysis. (Figure presented.).
Highly efficient one-pot synthesis, antimicrobial and docking studies of newer β-amino carbonyl derivatives catalyzed by silica sulfuric acid
El-Bayouki,Basyouni,El-Sayed,Tohamy,El-Henawy
, p. 255 - 268 (2013/01/15)
Mannich reaction was applied between 4-fluorobezaldehyde, selected acetophenone and several anilines, catalyzed by silica sulfuric acid for the synthesis of β-amino carbonyl derivatives. Reaction time and yield of the products depended on the nature of ac
Buchwald-Hartwig coupling/Michael addition reactions: One-pot synthesis of 1,2-disubstituted 4-quinolones from chalcones and primary amines
Fei, Xiang-Dong,Zhou, Zhou,Li, Wen,Zhu, Yong-Ming,Shen, Jing-Kang
experimental part, p. 3001 - 3008 (2012/07/13)
The Buchwald-Hartwig coupling/Michael addition sequence has been successfully applied to the synthesis of functionalized 1,2-disubstituted 4-quinolones using Pd(OAc)2 as a catalyst and PPh3 as a ligand. Under these conditions, the intermediate products first formed from chalcones and primary amines underwent catalytic dehydrogenation to yield the 1,2-disubstituted 4-quinolones. Copyright
